CA2998796A1 - Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer - Google Patents

Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer Download PDF

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Publication number
CA2998796A1
CA2998796A1 CA2998796A CA2998796A CA2998796A1 CA 2998796 A1 CA2998796 A1 CA 2998796A1 CA 2998796 A CA2998796 A CA 2998796A CA 2998796 A CA2998796 A CA 2998796A CA 2998796 A1 CA2998796 A1 CA 2998796A1
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Prior art keywords
substituted
mmol
phenyl
compound
amino
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Pending
Application number
CA2998796A
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English (en)
French (fr)
Inventor
Nicolas GUISOT
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Loxo Oncology Inc
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Loxo Oncology Inc
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Filing date
Publication date
Priority claimed from GBGB1516445.2A external-priority patent/GB201516445D0/en
Priority claimed from GBGB1522246.6A external-priority patent/GB201522246D0/en
Priority claimed from GBGB1613947.9A external-priority patent/GB201613947D0/en
Application filed by Loxo Oncology Inc filed Critical Loxo Oncology Inc
Publication of CA2998796A1 publication Critical patent/CA2998796A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
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    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Toxicology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Emergency Medicine (AREA)
CA2998796A 2015-09-16 2016-09-16 Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer Pending CA2998796A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GBGB1516445.2A GB201516445D0 (en) 2015-09-16 2015-09-16 Compounds
GB1516445.2 2015-09-16
GBGB1522246.6A GB201522246D0 (en) 2015-12-16 2015-12-16 Compounds
GB1522246.6 2015-12-16
GB1613947.9 2016-08-15
GBGB1613947.9A GB201613947D0 (en) 2016-08-15 2016-08-15 Compounds
PCT/GB2016/052897 WO2017046604A1 (en) 2015-09-16 2016-09-16 Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer

Publications (1)

Publication Number Publication Date
CA2998796A1 true CA2998796A1 (en) 2017-03-23

Family

ID=56985638

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2998796A Pending CA2998796A1 (en) 2015-09-16 2016-09-16 Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer

Country Status (15)

Country Link
US (3) US10611766B2 (es)
EP (2) EP3350184B1 (es)
JP (2) JP7337502B2 (es)
KR (1) KR20180109842A (es)
CN (2) CN108431007B (es)
AU (1) AU2016322063A1 (es)
CA (1) CA2998796A1 (es)
CL (1) CL2018000706A1 (es)
EA (1) EA201890730A1 (es)
ES (1) ES2929528T3 (es)
HK (1) HK1258779A1 (es)
IL (1) IL258154A (es)
MX (1) MX2018003351A (es)
PH (1) PH12018500587A1 (es)
WO (1) WO2017046604A1 (es)

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UA127863C2 (uk) 2015-12-16 2024-01-31 Локсо Онколоджі, Інк. Сполуки, які можна застосовувати як інгібітори кінази
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WO2023110970A1 (en) 2021-12-14 2023-06-22 Netherlands Translational Research Center Holding B.V Macrocyclic btk inhibitors
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GB201410430D0 (en) * 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
JP7337502B2 (ja) 2015-09-16 2023-09-04 ロクソ オンコロジー, インコーポレイテッド がんの治療のためのbtk阻害剤としてのピラゾロピリミジン誘導体
UA127863C2 (uk) 2015-12-16 2024-01-31 Локсо Онколоджі, Інк. Сполуки, які можна застосовувати як інгібітори кінази

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CN114685516A (zh) 2022-07-01
US10399989B2 (en) 2019-09-03
JP2023134428A (ja) 2023-09-27
CL2018000706A1 (es) 2018-07-13
CN108431007A (zh) 2018-08-21
US20180362533A1 (en) 2018-12-20
US10611766B2 (en) 2020-04-07
PH12018500587A1 (en) 2018-10-15
WO2017046604A1 (en) 2017-03-23
JP2018527384A (ja) 2018-09-20
MX2018003351A (es) 2018-09-17
CN108431007B (zh) 2022-06-07
EA201890730A1 (ru) 2018-10-31
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US20180362537A1 (en) 2018-12-20
EP3350184A1 (en) 2018-07-25
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AU2016322063A1 (en) 2018-04-12
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